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QuickView for Loratadine (compound)

Summary
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PubChem

PubChem Compound 3957

Name:	Loratadine
PubChem Compound ID:	3957
Description:	A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
Molecular formula:	C₂₂H₂₃ClN₂O₂
Molecular weight:	382.883 g/mol
Synonyms:	Clarityne; Claritin; NINDS_000792; Lorastine; Claratyne Cold; Loracert; Talorat Dy; Loratadine; Polaratyne; KBio1_000792. show more » Clarityne; Claritin; NINDS_000792; Lorastine; Claratyne Cold; Loracert; Talorat Dy; Loratadine; Polaratyne; KBio1_000792; KBio3_001520; Anhissen; Loradif; Lisino; SMR000058255; Claratyne; Pylor; Bedix Loratadina; Nularef; Claratyne Decongestant; Claritin D; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-, ethyl ester; Loratadina [Spanish]; Rinomex; D00364; KBio2_001976; Rhinase; Sensibit; EU-0100680; Spectrum4_000177; Spectrum_001496; Spectrum3_000740; Spectrum2_001584; Claritin (TN); Claritine; Lopac-L-9664; Loranox; Lorfast; KBioSS_001976; ZINC00537931; Allertidin; 79794-75-5; Aerotina; Loritine; KBio2_007112; SPBio_001548; Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylate; Tocris-1944; Lesidas; Clarityne Dy Repetabs; Lorantis; Loratadinum [Latin]; Zeos; Alerpriv; Sch 29851; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester; Sohotin; Loratyne; LS-114660; Bonalerg; Lertamine; KBioGR_000693; NCI60_041473; Tadine; Civeran; Fristamin; HSDB 3578; MLS000069647; Claritin reditab; 1-Piperidenecarboxylic acid, 4-(8-chloro-5,6-duhydro-11H-benzo [5, 6]cyclohepta[1,2-b]-pyridin-11-ylidene)-, ethyl ester; Biloina; Clarinase; NCGC00015619-01; Histaloran; Sanelor; Optimin; Clarityne-D; Loraver; Lowadina; Velodan; Sch-29851; DivK1c_000792; Alarin; Restamine; Sinhistan Dy; Loratadine [USAN:BAN:INN]; Loradex; Lergy; KBio2_004544; Clarityn; Clarinase Reperabs; Loratadine (JAN/USAN); NSC721075; NCGC00023125-02; Versal show less «

DrugBank

Identification

Name:	Loratadine
Name (isomeric):	DB00455
Drug Type:	small molecule
Description:	A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
Synonyms:	Loratadina [Spanish]; Loratadinum [Latin]
Brand:	Alarin, Sinhistan Dy, Pylor, Clarityn, Versal, Lorantis, Lomilan, Loracert, Rhinase, Loradif, Lergy, Zeos, Claritin-D, Sanelor, Restamine, Loradex, Fristamin, Loranox, Clarityne, Bonalerg, Lowadina, Lorfast, Rinomex, Claritin Reditabs, Loratyne, Allertidin, Talorat Dy, Clarinase, Lesidas, Bedix Loratadina, Claritine, Sohotin, Lertamine, Polaratyne, Alerpriv, Roletra, Tadine, Alavert, Claritin, Optimin, Clarinase Reperabs, Lisino, Lorastine, Nularef, Loraver, Biloina, Sensibit, Claratyne, Histaloran, Civeran, Velodan, Loritine, Aerotina
Brand name mixture:	Liberator(Loratadine + Pseudoephedrine Sulfate), Chlor-Tripolon ND SRT(Loratadine + Pseudoephedrine Sulfate), Claritin Allergy + Sinus Extra Strength(Loratadine + Pseudoephedrine Sulfate)
Category:	Antihistamines, Antipruritics, Anti-Allergic Agents, Histamine H1 Antagonists, Non-Sedating
CAS number:	79794-75-5

Pharmacology

Indication:	A self-medication that is used alone or in combination with pseudoephedrine sulfate for the symptomatic relief of seasonal allergic rhinitis. Also used for the symptomatic relief of pruritus, erythema, and urticaria associated with chronic idiopathic urticaria in patients (not for children under 6 unless directed by a clincian).
Pharmacology:	Loratadine is a long acting second generation antihistamine that is similar in structure to cyproheptadine and azatadine. The pharmacology of loratadine is similar to other antihistamines, but unlike other H₁-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H₁ receptors. The exact mec... show more » Loratadine is a long acting second generation antihistamine that is similar in structure to cyproheptadine and azatadine. The pharmacology of loratadine is similar to other antihistamines, but unlike other H₁-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H₁ receptors. The exact mechanism of this interaction is unknown, but disposition of the drug suggests that loratadine's prolonged antagonism of histamine may be due to the drug's slow dissociation from the receptor or the formation of the active metabolite, desloratadine. Loratadine does not penetrate the CNS effectively and has a low affinity for CNS H₁-receptors. show less «
Mechanism of Action:	Loratadine competes with free histamine and exhibits specific, selective peripheral H₁ antagonistic activity. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine. Loratadine has low affinity for cholinergic recept... show more » Loratadine competes with free histamine and exhibits specific, selective peripheral H₁ antagonistic activity. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine. Loratadine has low affinity for cholinergic receptors and does not exhibit any appreciable alpha-adrenergic blocking activity in-vitro. Loratadine also appears to suppress the release of histamine and leukotrienes from animal mast cells, and the release of leukotrienes from human lung fragments, although the clinical importance of this is unknown. show less «
Absorption:	Rapidly absorbed following oral administration (40% bioavailability)
Protein binding:	97-99%
Biotransformation:	Hepatic
Half Life:	8.4 hours
Toxicity:	somnolence, tachycardia, and headache LD₅₀=mg/kg (orally in rat)
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take on empty stomach: 1 hour before or 2 hours after meals.

Drug interaction:

Trospium	Trospium and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine	Triprolidine and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trimethobenzamide	Trimethobenzamide and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Nefazodone	Increased risk of cardiotoxicity
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Loratadine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.

Targets

Histamine H1 receptor

In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system

UniProt ID:

P35367

Gene:

HRH1

Actions:

antagonist

References:

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
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Cieslewicz G, Gondorowicz K, Grzelewska-Rzymowska I, Rozniecki J, Wojciechowska B: [Effect of loratadine--selective antagonist of histamine (H1) receptor--on allergen-induced bronchoconstriction in atopic asthmatics] Pneumonol Alergol Pol. 1992;60(11-12):11-5.
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Cieslewicz G, Gondorowicz K, Grzelewska-Rzymowska I, Rozniecki J: [Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction] Pneumonol Alergol Pol. 1995;63(5-6):281-5.
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Letari O, Miozzo A, Folco G, Belloni PA, Sala A, Rovati GE, Nicosia S: Effects of loratadine on cytosolic Ca2+ levels and leukotriene release: novel mechanisms of action independent of the anti-histamine activity. Eur J Pharmacol. 1994 Feb 15;266(3):219-27.
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Cavero I, Mestre M, Guillon JM, Heuillet E, Roach AG: Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Drug Saf. 1999;21 Suppl 1:19-31; discussion 81-7.
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Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology. 2005 Dec;75(1):45-52. Epub 2005 Jun 7.
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Grzelewska-Rzymowska I, Gondorowicz K, Cieslewicz G, Rozniecki J, Wojciechowska B: [Effect of loratadine (LO), a selective H1 antagonist, on histamine-induced bronchoconstriction] Pneumonol Alergol Pol. 1992;60(11-12):16-21.
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Menardo JL, Horak F, Danzig MR, Czarlewski W: A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4.
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Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41.
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Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27.
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Enzymes

Transporters

Multidrug resistance protein 1